Bioavailability of cyclosporine in rats after intragastric administration: a comparative study of the L2-phase and two other lipid-based vehicles

Transplant Immunology
M BojrupH Ekberg

Abstract

The purpose of this study was to evaluate formulations based on surface active dietary lipids only as oral vehicles for cyclosporine. The absolute bioavailability of cyclosporine from two new lipid vehicles was determined in rats after intragastric administration and compared to that of Sandimmun oral solution, which contains non-ionic surface active substances in addition to dietary lipids. In the new vehicles, cyclosporine was dissolved in two different mixtures of glycerides from long-chained fatty acids. One mixture forms an L2-phase, an oil with very low interfacial tension towards water, and was administered both as the oily L2-phase and as a predispersed emulsion formulation. The other mixture forms a liquid crystalline phase and was administered only as an aqueous dispersion. The mean bioavailability of cyclosporine from Sandimmun was 8% while it was 34% from the L2-phase, 38% from the predispersed L2-phase and 27% from the dispersed liquid crystalline phase. The coefficients of variation in area under the blood concentration curve after administration of the two formulations based on the L2-phase were quite low (31% for the L2-phase and 24% for the predispersed L2-phase) and comparable to that after intravenous adminis...Continue Reading

References

Feb 1, 1992·The Journal of Pharmacy and Pharmacology·S HedayatiM Rowland
Jul 1, 1992·British Journal of Clinical Pharmacology·J DreweK Gyr
Feb 1, 1991·Journal of Pharmacokinetics and Biopharmaceutics·A Bernareggi, M Rowland
Feb 1, 1989·Transplantation·L W ElzingaJ M Barry
Mar 1, 1986·Clinical Pharmacokinetics·R J PtachcinskiG J Burckart
Jan 1, 1986·European Journal of Clinical Pharmacology·J GrevelK Kutz
Jan 1, 1994·Biopharmaceutics & Drug Disposition·A Lindberg-Freijs, M O Karlsson
Jun 1, 1993·Clinical Pharmacokinetics·A Fahr

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Citations

Feb 21, 2003·International Journal of Pharmaceutics·Jung Yoon UmSeo Young Jeong
Jun 7, 2000·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·T Gershanik, S Benita

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